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PubMed1991

Influence of different sources on the processing and biopharmaceutical properties of high-dose ibuprofen formulations.

It is known that depending on the manufacturing and synthetic processes, drugs may exist as different forms. As a result, physicochemical properties, compression characteristics, intrinsic dissolution and bioavailability may vary substantially. The purpose of this study was to investigate the effect of different sources of ibuprofen on the processing of tablets and on their properties. Another emphasis of this work was to rationalize one or several key characteristics of the raw material as directly related to wet granulation parameters and to the behavior of final tablets. Commercially available ibuprofen was obtained from different manufacturers and a preformulation program, including X-ray crystallography, differential scanning calorimetry, scanning electron microscopy, determination of particle size distribution and flowability, was performed to characterize the raw material. Granules were prepared with a planetary mixer and liquid requirements for the end point were obtained by monitoring power consumption. Tablets were manufactured on Stokes rotary and single punch instrumented presses. Data acquisition interfaces produced compression data for each formulation. Granules and final tablets were analyzed for hardness, dissolution profiles and content uniformity. Statistical evaluations using analysis of variance and multiple comparison procedures were performed on the results to determine the significance of the variability between independent parameters. The ibuprofen tested was found to be a unique polymorphic form with some differences in the external crystallinity. The particle size characteristics of the material also allowed a differentiation between sources and although there was no differences in dissolution patterns or content uniformity, particle size was found to account for 50% of the variability in tablet hardness. Two sources of ibuprofen with lower mean particle size showed significant variations in end point liquid requirements resulting in variable tablet crushing strength.

Biopharmaceutics↗
PubMed1991

Biopharmaceutic evaluation of some 4-quinolone derivatives.

The relationships between physicochemical properties (ionization, solubility, partition, protein binding) of 4-quinolone derivatives and their pharmacokinetics was studied by means of in vitro methods. This information is needed to clarify the erratic absorption behaviour of quinolone antibacterials following oral administration. The ionization constants of ofloxacin (OF), pefloxacin (PF), norfloxacin (NF) and ciprofloxacin (CF) were determined by solubility, potentiometric, spectrophotometric, and octanol-water partition methods. The quinolones are ampholytes showing small values of partition coefficients (order of magnitude 1) resulting from their hydrophilic nature. Within the series, both partition coefficients and the ionization constants differ only slightly (5.5 less than pK1 less than 6.5, and 7.5 less than pK2 less than 8.5). The intrinsic solubility of nonionized forms of drugs was obtained to be of 1g/l order of magnitude. Linear relationship was observed between the log solubility versus reciprocal temperature. The dissolution of NF is an endothermic reaction with dissolution enthalpy H = 20.4 kJ/mol. In vitro diffusion of OF, PF, NF, and CF was studied by the means of Sartorius in vitro absorption model. The rate of diffusion and the projected in vitro rate of absorption are not functions of structural differences within the series (diffusion rate constant range was 0.5 less than kd less than 5.0 .10-3 cm/min). Binding of NF, CF, PF and OF to bovine serum albumin (BSA) was studied using equilibrium dialysis in the absence and presence of urea. It was found that the quinolones were moderately bound (40-60%) to BSA and that urea in pathologic concentrations diminished their binding for 10-25%.

4-Quinolones↗
PubMed1990

Biopharmaceutic aspects of buccal absorption of insulin.

Absorption of insulin through buccal mucosa was investigated using rabbits as animal model. The effects of various dose sizes, pH of the insulin solutions and a series of sorption enhancers or absorption promoters on the hypoglycemic response were studied using a buccal cell. In the absence of sorption promoters, the various dose sizes and pH of the administered insulin solution did not show any significant hypoglycemic response, indicating that substantial amounts of insulin were not absorbed through the buccal mucosa. In the presence of sorption enhancers, the extent of hypoglycemia was significantly enhanced in terms of AUC and Cmax. Among the sorption enhancers investigated, Brij 35 was the most satisfactory one, followed by sodium taurocholate, sodium laurylsulfate, sodium deoxycholate, sodium methoxysalicylate, sodium dextransulfate and EDTA. An inverse correlation was found between extent of hypoglycemia and light scattering intensity of insulin solution. The extent of hypoglycemia in presence of Brij 35 was concentration-dependent although a plateau was observed at high concentration range. The maximum pharmacological availability obtained from buccal administration of insulin solution was about 12%, while that obtained with the tablet formulation was about 4.3%.

Administration, Buccal↗
PubMed1990

[Biopharmaceutic studies of a bioerodible nystatin unit].

The release of nystatin from monolithic bioerodible system with pectin was studied. The process of both system degradation and drug release was expressed with an equation of Hixon and Crowell. It was established that an increasing thickness of the system as well as an increase of drug concentration decreased the rate of erosion and the release of the active principle. Both the concentration of the plastificator and the temperature of drying the system in the range of investigation did not change these processes.

Biopharmaceutics↗
PubMed1989

Biopharmaceutical comparison of two levothyroxine sodium products.

The relative bioavailability and therapeutic equivalence of two brands of levothyroxine sodium tablets, Levothroid and Synthroid, were compared in patients who had been receiving long-term levothyroxine replacement therapy. Eighteen patients with primary hypothyroidism were randomly assigned to receive therapeutic dosages of Levothroid or Synthroid for 43 days and then were switched to the opposite product for 43 more days. The pharmacokinetic profiles of the two drugs were evaluated on days 43 and 86 by analyzing blood samples drawn at various intervals after the final dose. Relative bioavailability was determined by comparing the absorption profiles and areas under the serum concentration-time curves (AUCs) of total and free serum thyroxine. In addition, the potency of the levothyroxine sodium tablets was determined by high-performance liquid chromatography. The time to reach maximum concentration and the maximum concentration of total thyroxine after treatment with Levothroid did not differ significantly from those after treatment with Synthroid. The mean +/- S.D. AUC of total thyroxine after Levothroid administration (2339 +/- 404 pg.hr/mL) was slightly but significantly higher (p = 0.047) than that following Synthroid (2169 +/- 422 pg.hr/mL). However, the main index of biological activity, thyrotropin concentration, did not differ significantly between the two products. All tablets tested were within the stated potency requirements of the USP. The AUC of total serum thyroxine and the serum thyrotropin concentration after long-term replacement therapy with Levothroid or Synthroid indicate that any differences in bioavailability between the two products are clinically unimportant and that the two products are therapeutically interchangeable.

Adult↗
PubMed1989

Quantitative determination of verapamil and metabolites in human serum by high-performance liquid chromatography and its application to biopharmaceutic investigations.

A specific and sensitive high-performance liquid chromatographic method for the quantitative analysis of verapamil and N-desmethylverapamil in human serum is described. The analytes were extracted from serum using diethylether under alkaline conditions, followed by back extraction into dilute hydrochlorid acid for chromatographic analysis on a reversed-phase column with a mobile phase consisting of acetonitrile, water and perchloric acid at a flow rate of 1 l/min. The analytes were detected by fluorescence detection, the influence of temperature on retention is discussed. The method is linear, quantitative and reproducible for two calibration ranges in serum (2.5 ng/ml-100 ng/ml and 12.5 ng/ml-500 ng/ml) using peak area ratios analyte/internal standard for quantification. At ultimate sensitivity, concentrations down to 250 pg/ml could be assayed. The method was selective to 6 other metabolites of verapamil and common exogenous interferences. It was applicated to the serum samples of a comparative 120 mg - verapamil hydrochloride tablet single dose two-way cross-over study comprising 18 volunteers. The pharmacokinetic data for both formulations are presented.

Biopharmaceutics↗